917562-33-5

JT010 is a transient receptor potential ankyrin 1 (TRPA1) agonist (EC₅₀ = 0.65 nM in a calcium influx assay). It is selective for TRPA1 over TRP vanilloid 1 (TRPV1), TRPV3, TRPV4, TRP canonical channel 5 (TRPC5), TRP melastatin 2 (TRPM2), and TRPM8 channels at 1 μM.

JT010 is a potent and selective TRPA1 channel activator (EC50 = 65 nM); activates the TRPA1 channel by covalently and site-selectively binding to Cys621. Exhibits selectivity for TRPA1 over TRPV1, TRPV3, TRPV4, TRPM2, TRPM8, and TRPC5 channels (EC50 values are >1 μM).

JT010 is a non-cytotoxic and highly stable (>90% remains after 2 h in 1 mM DTT or 2-mercaptoethanol) chloroacetamido warhead-carrying thiazole derivative that acts as a potent and TRPA1-selective channel activator via covalent modification of TRPA1 active site Cys621. JT0101 stimulates calcium influx in TRPA1-transfected HEK293 cells in a dose-dependent manner (EC50?= 650 pM) with excellent selectivity over TRPV1, TRPV3, TRPV4, TRPM2, TRPM8, and TRPC5 channels (EC50?>1 μM).

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[1] JUNICHIRO TAKAYA. A Potent and Site-Selective Agonist of TRPA1[J]. Journal of the American Chemical Society, 2015, 137 50: 15859-15864. DOI: 10.1021/jacs.5b10162